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Synthesis and biological activity of O-alkyl-3-N-aminoacyloxymethyl-5- fluoro-2'-deoxyuridine derivatives

DOI: 10.1248/cpb.44.1196

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1196 - 1201 (1996)

Update date:2022-08-05

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Authors:

Harada, NaoyukiHarada, Naoyuki

Hongu, MitsuyaHongu, Mitsuya

Kawaguchi, TakayukiKawaguchi, Takayuki

Ohohashi, MotoakiOhohashi, Motoaki

Oda, KoujiOda, Kouji

Hashiyama, TomikiHashiyama, Tomiki

Tsujihara, KenjiTsujihara, Kenji

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Article abstract of DOI:10.1248/cpb.44.1196

In an attempt to improve the effectiveness of action of 5-fluoro-2'- deoxyuridine (FUdR), various kinds of O-alkylated water-soluble analogues were synthesized. Antitumor activities against sarcoma 180 (solid) were also evaluated. Some compounds exhibited potent activities. In particular, 3'-O- p-chlorobenzyl-3-N-aminoacyloxy-methylester derivatives were effective over a very wide range of dose and gave extremely large therapeutic ratios compared with known 5-fluorouracil (5-FU) derivatives.

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Full text of DOI:10.1248/cpb.44.1196

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Products guided by the article

Product name:3-tert-Butoxycarbonylamino-propionic acid 3-[(2R,4S,5R)-4-(4-chloro-benzyloxy)-5-hydroxymethyl-tetrahydro-furan-2-yl]-5-fluoro-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-ylmethyl ester

Cas No:179744-31-1

179744-31-1

R&D Labs maybe for 179744-31-1

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